Penetration of levofloxacin into lung tissue after oral administration to subjects undergoing lung biopsy or lobectomy.
OBJECTIVE
To evaluate the pulmonary tissue distribution of levofloxacin, the new once-daily fluoroquinolone, after a single 500-mg oral dose.


METHODS
Open-label study.


METHODS
One pulmonary clinic and two university-affiliated teaching hospitals.


METHODS
Eighteen adults undergoing lung biopsy or lobectomy.


METHODS
Levofloxacin plasma and lung tissue concentrations were determined by high-performance liquid chromatography with fluorescence detection. Lung tissue levofloxacin concentrations were corrected for blood contamination by measuring hemoglobin.


RESULTS
After a single 500-mg oral dose, concentrations of levofloxacin in lung tissue consistently exceeded those in plasma at every time point over the 24-hour sampling period, with tissue:plasma penetration ratios of 2.02 (2-3 hrs), 5.02 (4-6 hrs), 5.13 (11-17 hrs), and 4.13 (22-25 hrs). The mean penetration ratio over the 24-hour sampling period was 3.95 (range 1.06-9.98). Lung tissue concentrations of levofloxacin also exceeded minimum inhibitory concentration values for most community-acquired respiratory tract pathogens over the 24 hours.


CONCLUSIONS
This study supports clinical evaluation of levofloxacin as once-daily oral therapy for community-acquired lower respiratory tract infections.
Lee
L J
LJ
Global Clinical Pharmacology Department, Hoechst Marion Roussel Inc, Bridgewater, New Jersey 08807-0880, USA.
Sha
X
X
Gotfried
M H
MH
Howard
J R
JR
Dix
R K
RK
Fish
D N
DN
D000284:Administration, Oral; D000368:Aged; D000890:Anti-Infective Agents / Q000009:adverse effects / Q000378:metabolism*; D001706:Biopsy; D005260:Female; D006801:Humans; D064704:Levofloxacin; D008168:Lung / Q000378:metabolism* / Q000473:pathology; D008297:Male; D008875:Middle Aged; D009325:Nausea / Q000139:chemically induced; D015242:Ofloxacin / Q000009:adverse effects / Q000378:metabolism*; D011013:Pneumonectomy
D000890:Anti-Infective Agents; D064704:Levofloxacin; D015242:Ofloxacin